1. Field of the Invention
The invention relates to biologically active food supplements to restore sex drive (libido) and improve sexual function in male and is based on natural ingredients.
2. Description of Related Art
Sexual dysfunction, including decreased libido, erectile and ejaculation dysfunction, as well as infertility, are widespread medical, psychological, and social problems.
Today, there exists quite a few pharmaceutical drugs—inhibitors of phosphodiesterase of type 5 (PDEI-5), such as Viagra, Cialis, Zidena, Levitra, for treating sexual dysfunctions. At the same time, the high cost of these drugs and significant risk of adverse drug reactions, especially in patients with cardiovascular disease, limit their widespread use. In addition, there are patients (15-42%) in which PDEI-5 are inefficient due to the mechanism of action of this group of drugs. It is known that these drugs can potentiate NO relaxing action on smooth muscle tissue of trabecular cells. However, the starting point for NO release from nerve endings is the impulses coming from the central nervous system. Their intensity depends on the patient's response to sexual stimuli, i.e. evidence of sex drive or libido. With a sharp decrease of libido (this is it that fades with age in the first place), monotherapy with PDES inhibitors is ineffective due to lack of substrate for their actions (Segraves K. B., Segraves R. T., Hypoactive sexual desire disorder: prevalence and comorbidity in 906 subjects, J Sex Marital Ther, 1991, Vol. 17, pp. 55-58; Pushkar D. Yu., Yudovsky S. O., Combined use of Enerion (sulbutiamin) and Cialis (tadalafil) in therapy of patients with erectile dysfunction, 2007—http://medi.ru/doc/a0210603.htm).
As far as androgen replacement therapy (ART) employing testosterone preparations used per os, intramuscularly, or percutaneously) is concerned, there left a number of unresolved problems despite the variety of dosage forms. Firstly, none of the drugs is able to precisely reproduce a circadian rhythm in the serum testosterone level. Secondly, a number of studies have shown that exogenous increase of testosterone has a greater influence on the erectile function rather than on sexual-erotic, libidinal component, this being caused by a visceral defect of hypothalamic brain structures. Thirdly, androgens are potentially able to have adverse effects not only due to cutting off its own mechanisms of androgen production but also due to affecting homeostasis maintaining systems suppressing the production of endogenous androsteroids. Side effects primarily affect the prostate gland, lipid profile, cardiovascular system, hematologic state, sleep system, social behavior, and emotional status (Pushkar′ D. Yu., Segal A. S., Yudovsky S. O., Current opportunities for androgen replacement therapy in cases of male hypogonadism, Pharmaceutical Bulletin, 2008, No. 13, p. 33). When administering ART, one should ensure the functional safety of the liver to avoid final catabolism disorders with increased levels of estrogen that provokes release of inhibiting substances able to block achievable, albeit usually modest, positive therapeutic results.
Impaza—a preparation containing antibodies to human endothelial NO-synthase. The main mechanism of its action is to enhance the activity of endothelial NO-synthase, to recover production of nitric oxide (NO) by endothelium, and to increase the cGMP content in smooth muscles and to relax same that leads to a rising of blood supply to the corpus cavernosum. These effects primarily recover erection. With regard to libido, target studies have not been conducted; according to individual data, the increase of libido is less than 20% (Neumark A. I., Simashkevich A. V., Aliyev R. T., Treating patients with prostate benign hyperplasia complicated by the erectile dysfunction, Attending physician, 2010, No. 4, pp. 89-91).
The closest analogue to the proposed supplement are formulations that are useful in the treatment of male and female impotence; they are based on extracts of Tribulus terrestris, Epimedium koreanum and Cinnamon cassia combined in a specific weight ratio, and optionally contain arginine or physiologically equivalent ester, its salt or precursor and suitable carrier or excipient (patent of the Russian Federation No 2313358, 2003).
The effect of this composition on libido is low. It is primarily aimed at the elimination of erectile dysfunction. Another disadvantage of this composition is the use of a medicinal plant Tribulus terrestris, which is prohibited by Rospotrebnadzor (a Russian analog of the FDA) for using as a raw material for the production of biologically active additives to food because of the high toxicity of this plant.
Offered in this application is a food supplement to restore/enhance libido with the following daily dosage composition shown in ranges:
ComponentsMg of active substanceSaponins from true or false ginseng rootsfrom 5 mg to 20 mgEcdysteroids from Leuzea rootfrom 0.1 mg to 30 mgL-ArginineFrom 300 mg to 1,000 mgIcariin from Horny goat weedFrom 20 to 150 mgDecenoic acids from male bee broodfrom 0.4 mg to 1 mgRutin from pollen or beebreadfrom 40 mg to 100 mgZinc from zinc citratefrom 6 mg to 60 mgVitamin B6from 0.3 mg to 3 mg,the upper limit being selected due to toxicity, the lower limit—due to effectiveness.
L-Arginine is a protein-forming amino acid. It is a source of adequate forming of nitric oxide (NO) by vascular endothelium, which is associated with the dependent relaxation of smooth muscle cells of cavernous tissue determining the hemodynamic changes in the penis during erection and rigidity phase (K. E. Anderson, Pharmacology of penile erection, Pharmacol. Rev., 2001, 53 (September (3): 417-50.). L-arginine has a stimulating effect on the reproductive system: it increases the production of seminal fluid and spermatogenesis; stimulates the potency and sexual activity; can increase the strength and duration of genitals blood filling; prolongs the duration of sexual intercourse; enhances pleasant sexual sensations; makes orgasms last longer; increases the frequency and intensity of orgasms. It improves mood, activity and endurance.
Horny Goat Weed contains icariin—flavonol derived from plants of Epimedium family, which are widely known as Horny Goat Weed (literally—an herb of a horny goat). The extract of Epimedium for centuries has been used in Chinese traditional medicine to treat impotence and improve sexual function.
The mechanism of its action is similar to a phosphodiesterase inhibitor. It increases the production of nitric oxide, improves circulation and myotrophy. It is tropic to androgen receptors and acts like testosterone, causing accelerated growth of muscle tissue, increases sex drive and endurance. Horny Goat Weed extract has antioxidant, antidepressant and nootropic effects.
Male bee brood (male bee-brood homogenate) is a natural substance which contains natural testosteroids, progesterone and estradiol. Male bee brood restores metabolism and nutrition of tissues, helps stabilize blood pressure, has a regulating effect on the tone of the vascular system and the level of blood circulation, lowers blood cholesterol level. It promotes the accelerated recovery of biochemical and mass-metric characteristics of testes and prostate. As a stimulant of the central mechanisms of regulation of androgen formation, it increases physical performance, helps restore impaired sexual function in males and increase sexual desire.
Pollen or beebread are male plant cells, a natural concentrate containing proteins, all essential amino acids, carbohydrates, lipids, minerals and microelements (potassium, calcium, phosphorus, iron, magnesium, manganese, chromium, zinc, iodine, etc.), vitamins (carotenoids, C, D, E, groups B, P, PP, K, et al.), phytohormones and flavonoids. Pollen restores liver function, lowers the level of blood sugar, normalizes the process of digestion; stimulates the adrenal glands, lowers blood cholesterol; normalizes blood pressure; increases stress resistance, mental and physical performance.
Zinc citrate—zinc has a strong immunostimulatory effect. It actively influences the state of the sexual function in men: it is a building material for testosterone, increases activity of sperm cells, promotes proper functioning of male sex glands. Zinc deficiency plays a key role in the development of benign prostatic hyperplasia (adenoma) (BPH) where the activation of the 5-alpha-reductase enzyme occurs, which converts testosterone into dihydrotestosterone (DHT). The level of testosterone in blood decreases, DHT accumulates in the prostate gland which leads to prostate enlargement. Whereas high content of zinc contributes to blocking this process. It has psychotropic (improves mood, reduces irritability, improves memory and attention) and antioxidant actions. Zinc citrate is available as dihydrate and trihydrate and is produced by complete neutralization of citric acid with a high purity zinc source, subsequent precipitation and dehydration.
Vitamin B6 normalizes hormonal balance, enhances immunity, improves the heart function, restores the function of prostate cells. It plays a significant role in the treatment of infertility and in energy processes occurring in spermatozoa, especially where their mobility is reduced.
True or false ginseng root has adaptogenic, bio-stimulating, and tonic effects. Its pharmacological activity results from having saponin glycosides and ginsenoides, fatty and ester oils, sterols, peptides, vitamins and minerals. The active ingredients of ginseng improve prostate function and sexual activity, actively influence the central nervous system, increase working capacity, and reduce physical and mental fatigue. In addition, ginseng improves the functional activity of cardiovascular system and regulates blood pressure.
Leuzea root has tonic and stimulant properties. The main pharmacological properties are the increase of muscle strength and performance, improvement of blood supply to muscles and brain. On long-term ingestion, it reduces morbidity, improves self-reported health, increases static endurance, improves mental and physical performance.
As one could see, none of the proposed components of the proposed composition has a pronounced effect on the libido increase. Any two, three, four or five components of the proposed composition do not substantially increase libido either.
It was established during research that only the combination of those components and only in that range can significantly increase libido, by 20-43% which is sufficient to amount to significantly more than the judicial exception and to make it protectable in terms of 35 U.S.C. §101. In other words, the tests revealed features sufficient to produce the desired synergistic effect.
Increasing libido even by 20% is significant as not all known drugs that enhance sexual activity can increase libido even up to 20%.
The libido level is a determining factor in male sexual activity, potency preservation, physiological and mental health.
In the study of “Remedy 1”, significant improvement of neurohumoral and mental components of the male copulative cycle was revealed resulting in the enhancement/restoration of libido and overall satisfaction with sexual relations in the studied males.
A positive correlation was established between the increase of androgen concentration in blood (for total testosterone and dehydroepiandrosterone sulfate) and a significant libido increase (by 42.8%) in men which indicates that the preparation has a central hypothalamic-pituitary mechanism of action. It is assumed that androgens enhance desire by increasing the sensitivity of the pleasure centers in the limbic system and hypothalamus, as well as by increasing overall activity and vitality of the body due to the stimulating effect of androgens on metabolism.
The central mechanism of action of the preparation is confirmed by the decrease of prolactin level in blood serum (from 548±136 to 24.5-467 mU/l, p<0.02) and the demonstration of anti-stress, psycho-stabilizing effects, as well as by the increase of libido, sexual activity due to the stimulating action of LH on Leydig cells secreting testosterone.
The claimed supplement is made in powder, tableted or capsuled forms and may also have a form of alcohol water extract and forms based on such an extract, namely, powder, tablets and capsules.